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头孢洛林加阿维巴坦在一室药代动力学/药效学模型中对致病性厌氧菌具有杀菌活性。

Ceftaroline plus avibactam demonstrates bactericidal activity against pathogenic anaerobic bacteria in a one-compartment in vitro pharmacokinetic/pharmacodynamic model.

机构信息

Anti-Infective Research Laboratory, Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit, Michigan, USA.

出版信息

Antimicrob Agents Chemother. 2014;58(1):559-62. doi: 10.1128/AAC.01358-13. Epub 2013 Nov 11.

Abstract

Anaerobic pathogens are often associated with polymicrobial infections, such as diabetic foot infections. Patients with these infections are often treated with broad-spectrum, multidrug therapies targeting resistant Gram-positive bacteria, such as methicillin-resistant Staphylococcus aureus, as well as Gram-negative bacteria and anaerobes. The broad-spectrum, non-beta-lactam, beta-lactamase inhibitor avibactam has been combined with ceftaroline and may provide a single-product alternative for complicated polymicrobial infections. We compared the activity of ceftaroline-avibactam (CPA) to that of ertapenem (ERT) against common anaerobic pathogens in an in vitro pharmacokinetic/pharmacodynamic (PK/PD) model. Simulations of doses of ceftaroline-fosamil at 600 mg every 8 h (q8h) (maximum free drug concentration [fCmax], 17.04 mg/liter, and half-life [t1/2], 2.66 h) plus avibactam at 600 mg q8h (fCmax, 11.72 mg/liter, and t1/2, 1.8 h) and of ertapenem at 1 g q24h (fCmax, 13 mg/liter, and t1/2, 4 h) were evaluated against two strains of Bacteroides fragilis, one strain of Prevotella bivia, and one strain of Finegoldia magna in an anaerobic one-compartment in vitro PK/PD model over 72 h with a starting inoculum of ∼8 log10 CFU/ml. Bactericidal activity was defined as a reduction of ≥3 log10 CFU/ml from the starting inoculum. Both CPA and ERT were bactericidal against all four strains. CPA demonstrated improved activity against Bacteroides strains compared to that of ERT but had similar activity against Finegoldia magna and P. bivia, although modest regrowth was observed with CPA against P. bivia. No resistance emerged from any of the models. The pharmacokinetics achieved were 92 to 105% of the targets. CPA has potent in vitro activity against common anaerobic pathogens at clinically relevant drug exposures and may be a suitable single product for the management of complicated polymicrobial infections.

摘要

厌氧病原体常与多种微生物感染相关,如糖尿病足感染。这些感染的患者通常接受广谱、多药物治疗,针对耐药革兰阳性菌,如耐甲氧西林金黄色葡萄球菌,以及革兰阴性菌和厌氧菌。非β-内酰胺类、β-内酰胺酶抑制剂阿维巴坦与头孢洛林联合使用,可能为复杂的多微生物感染提供一种单一产品的替代选择。我们在体外药代动力学/药效学(PK/PD)模型中比较了头孢洛林-阿维巴坦(CPA)与厄他培南(ERT)对常见厌氧病原体的活性。模拟头孢洛林-磷酸酯 600 mg 每 8 小时(q8h)(游离药物最大浓度 [fCmax],17.04 毫克/升,半衰期 [t1/2],2.66 小时)加阿维巴坦 600 mg q8h(fCmax,11.72 毫克/升,半衰期 [t1/2],1.8 小时)和厄他培南 1 g q24h(fCmax,13 毫克/升,半衰期 [t1/2],4 小时)的剂量对两种脆弱拟杆菌株、一种普雷沃氏菌属 bivia 株和一种金氏金杆菌株在 72 小时内的厌氧一室体外 PK/PD 模型中的活性进行了评估,起始接种量为约 8 log10 CFU/ml。杀菌活性定义为从起始接种量减少≥3 log10 CFU/ml。CPA 和 ERT 对所有四种菌株均具有杀菌活性。与 ERT 相比,CPA 对拟杆菌属菌株的活性得到改善,但对金氏金杆菌和普雷沃氏菌属 bivia 的活性相似,尽管 CPA 对普雷沃氏菌属 bivia 观察到适度的再生长。没有从任何模型中出现耐药性。达到的药代动力学为目标的 92%至 105%。CPA 在临床相关药物暴露时对常见厌氧病原体具有强大的体外活性,可能是治疗复杂多微生物感染的合适单一产品。

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